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Screening method for developing drugs against pathogenic microbes having two-component system

机译:具有两组分系统的抗病原微生物药物的筛选方法

摘要

The present invention relates to a package of screening methods for developing drugs against pathogenic microbes having two-component system of DevR-DevS and/or DevR-Rv2027c and its homologues, said method comprising steps of over-expressing DevR, DevS, and Rv2027c and their single domain derivatives including mutant variant proteins, autophosphorylating DevS, and Rv2027c proteins and thereafter, phosphotransfering to DevR and its derivatives in SDS-PAGE or High-throughput format in the presence of a test compound, and determining the drug-potential of the test compound, wherein the potential of the drug is inversely proportional to (i) the degree of autophosphorylation of DevS and Rv2027c, (ii). the degree of phosphotransfer-based dephosphorylation of DevR and/its single domain derivative, and (iii). the degree of dephosphorylation of phosphorylated species of DevS and Rv2027c and/their single domain derivatives, and a method of treatment, and a composition thereof.
机译:本发明涉及用于开发针对具有DevR-DevS和/或DevR-Rv2027c及其同系物的双组分系统的病原微生物的药物的筛选方法的包装,所述方法包括过表达DevR,DevS和Rv2027c的步骤,以及它们的单域衍生物,包括突变变体蛋白,自身磷酸化DevS和Rv2027c蛋白,然后在存在测试化合物的情况下以SDS-PAGE或高通量格式磷酸转移至DevR及其衍生物,并确定测试的药物潜力化合物,其中药物的潜力与(i)DevS和Rv2027c的自磷酸化程度成反比,(ii)。 DevR和/或其单域衍生物的基于磷酸转移的去磷酸化程度,以及(iii)。 DevS和Rv2027c和/或其单结构域衍生物的磷酸化物种的去磷酸化程度,治疗方法及其组合物。

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